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SEDATIVE-HIPNOTICE

SEDATIVE-HIPNOTICE. Clasificare: Sedative hipnotice barbiturice Sedative hipnotice nebarbiturice. SEDATIVE HIPNOTICE BARBITURICE Acizi slabi, derivati ai acidului barbituric/tiobarbituric; Farmacocinetica: Barbituricele liposolubile; Barbituricele < liposolubile;

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SEDATIVE-HIPNOTICE

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  1. SEDATIVE-HIPNOTICE

  2. Clasificare: • Sedative hipnotice barbiturice • Sedative hipnotice nebarbiturice

  3. SEDATIVE HIPNOTICE BARBITURICE Acizi slabi, derivati ai acidului barbituric/tiobarbituric; Farmacocinetica: • Barbituricele liposolubile; • Barbituricele < liposolubile; • Metabolizarea: hepatica → metaboliti inactivi

  4. Actiune farmacodinamica: 1. Sedative (doze mici); 2. Hipnotice (doze mari); 3. Narcotice: Tiopental (i.v.); 4. Anticonvulsivante: Fenobarbital; 5. Inductor enzimatic: Fenobarbital.

  5. Mecanism de actiune: barbiturice-benzodiazepine

  6. Utilizari terapeutice. • stari de hiperexcitabilitate, tireotoxicoza; • insomnii: - Ciclobarbitalul - Fenobarbitalul • epilepsie: - Fenobarbitalul

  7. Principii de administrare: • doza minima eficace; • administrare intermitenta; • durata administrarii: maximum 4 saptamani; • nu se intrerupe brusc tratamentul: risc de revenire (rebound) a insomniei.

  8. Efecte adverse: • agitatie psihomotorie (la batrani); • obisnuinta si dependenta; • intoxicatia acuta (supradozaj). Tratamentul intoxicatiei acute: - spalatura gastrica; - Manitol, alcalinizante (perfuzie i.v.); - respiratie asistata.

  9. Barbiturice. Contraindicatii: - porfirie; - insuficienta respiratorie severa; - soferi; - sindrom depresiv; - sarcina.

  10. II. SEDATIVE HIPNOTICE NEBARBITURICE DERIVATI DE BENZODIAZEPINA

  11. Actiune farmacodinamica: - anxiolitica - sedativa-hipnotica; - miorelaxanta; - anticonvulsivanta. Utilizari terapeutice: - insomnie anxioasa.

  12. ZOLPIDEM si ZOPICLONA Actiune farmacodinamica: - sedativa; - hipnotica; - anxiolitica; - anticonvulsivanta (Zopiclona); - miorelaxanta. Utilizari terapeutice: insomnii

  13. Zolpidem si Zopiclona Efecte adverse: - Zopiclona: gust amar si metalic; - toleranta si dependenta, nesemnificative. Administrare: 1 cpr seara

  14. TRANCHILIZANTE MINORE (ANXIOLITICE)

  15. Clasificare: • Derivati de benzodiazepina: DIAZEPAM, CLORDIAZEPOXID, OXAZEPAM, MEDAZEPAM, LORAZEPAM, BROMAZEPAM, CLOBAZAM, TOFISOPAM, etc…. B. Derivati de difenilmetan: HIDROXIZIN C. Carbamati ai propandiolului: MEPROBAMAT D. Derivat de azaspirodecandiona: BUSPIRONA

  16. BENZODIAZEPINELE: Farmacocinetica: • absorbtie buna din intestin; • fixare foarte buna pe proteine plasmatice; • difuzeaza bine in creier; • traverseaza placenta; • metabolizare hepatica → metabolit activ; • eliminare renala.

  17. BENZODIAZEPINELE: Actiune farmacodinamica: - anxiolitica; - sedativa; - hipnogena; - miorelaxanta; - anticonvulsivanta (Diazepam); - anestezica generala (Midazolam). Potenteaza deprimantele SNC, alcoolul etilic → NU se asociaza !!!

  18. Mecanism de actiune: barbiturice-benzodiazepine

  19. BENZODIAZEPINELE: Utilizari terapeutice: - sindrom anxios; - stari de neliniste, anxietate; - contracturi musculare; - preanestezie; - medicatie adjuvanta.

  20. BENZODIAZEPINELE

  21. BENZODIAZEPINE Principii de administrare: • initial, doze mici; • in anxietate acuta: BDZ cu actiune rapida; • in anxietate cronica: BDZ cu efect prelungit; • tratamentul nu se intrupe brusc; • la virstnici doze reduse (Oxazepam, Lorazepam).

  22. BENZODIAZEPINE

  23. TRANCHILIZANTE NEBENZODIAZEPINICE 1.HIDROXIZINA 2. MEPROBAMAT 3. BUSPIRONA

  24. BUSPIRONA Caracteristici farmacodinamice: • efect anxiolitic puternic: anxiolitic selectiv; • efect sedativ slab; NUeste miorelaxant/anticonvulsivant ! Administrare: oral, cpr.

  25. TRANCHILIZANTE MAJORE (NEUROLEPTICELE)

  26. NEUROLEPTICELE SEDATIVE Clasificare: • Neuroleptice fenotiazinice: CLORPROMAZINA, LEVOMEPROMAZINA, TIORIDAZINA, PERICIAZINA 2. Neuroleptice tioxantenice: CLORPROTIXEN, CLOPENTIXOL, FLUPENTIXOL 3. Neuroleptice butirofenonice: FLUANISONA

  27. NEUROLEPTICE FENOTIAZINICE CLORPROMAZINA Actiune farmacodinamica: - antipsihotica; - sedativa; - deprima SNV; - antivomitiva; - hipotermizant; - manifestari de tip extrapiramidal; - efecte endocrine.

  28. Clorpromazina Mecanism de actiune: Blocheaza: - receptorii dopaminergici D2 - receptorii adrenergici α1 si β - receptorii serotoninergici 5-HT2 - receptorii histaminergici H1

  29. Clorpromazina Utilizari terapeutice: - psihoze; - varsaturi; - sughit rebel; - preanestezie; - stari de hiperexcitabilitate.

  30. Clorpromazina Efecte adverse: - somnolenta; - hTA ortostatica; - manifestari extrapiramidale Administrare: Clordelazin dj. Plegomazin f. (i.m./i.v.)

  31. NEUROLEPTICE TIOXANTENICE -CLORPROTIXEN - CLOPENTIXOL - FLUPENTIXOLantipsihotic polivalent

  32. NEUROLEPTICE INCISIVE “antideficitare” sau “dezinhibitorii” Clasificare: • Fenotiazine: Flufenazina • Tioxantene: Tiotixen • Butiroferone: HALOPERIDOL, Pimozid, Penfluridol • Diverse: Sulpirida, Tiaprida

  33. HALOPERIDOL • neuroleptic incisiv cu potenta mare Actiune farmacodinamica: - antipsihotica marcata; - antivomitiva puternica; - sedativa moderata. Utilizari terapeutice: • psihoze acute si cronice; • agitatie psiho-motorie; • in anesteziologie • varsaturi

  34. Haloperidol Efecte adverse: • manifestari extrapiramidale intense • hTA ortostatica; • tulburari de vedere; • hipertermie. Administrare: cpr., f. (i.m., i.v., s.c.) Haloperidol decanoat f. (i.m.)

  35. Contraindicatii: - Parkinson; - scleroza in plagi; - epilepsie; - afectiuni hepatice grave; - sarcina - CONSUMUL DE ALCOOL !!!

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